The novel compound (±)-1-[10-((E)-3-Phenyl-allyl)-3,10-diaza-bicyclo[4.3.1]dec-3-yl]-propan-1-one (NS7051) attenuates nociceptive transmission in animal models of experimental pain; a pharmacological comparison with the combined μ-opioid receptor agonist and monoamine reuptake inhibitor tramadol

2008 ◽  
Vol 54 (2) ◽  
pp. 331-343 ◽  
Author(s):  
Gordon Munro ◽  
Camilla Æ. Bæk ◽  
Helle K. Erichsen ◽  
Alexander N. Nielsen ◽  
Elsebet Ø. Nielsen ◽  
...  
Keyword(s):  
Animal Models ◽  
Opioid Receptor ◽  
Reuptake Inhibitor ◽  
Receptor Agonist ◽  
Experimental Pain ◽  
The Novel ◽  
Nociceptive Transmission ◽  
Opioid Receptor Agonist ◽  
Μ Opioid Receptor

scholarly journals Four stereoisomers of the novel μ-opioid receptor agonist tapentadol hydrochloride

2011 ◽  
Vol 67 (2) ◽  
pp. o71-o76 ◽  
Author(s):  
Krishnan Ravikumar ◽  
Balasubramanian Sridhar ◽  
Nitin Pradhan ◽  
Mayur Khunt
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
The Novel ◽  
Opioid Receptor Agonist ◽  
Μ Opioid Receptor

In VitroBinding and Signaling Profile of the Novel μ Opioid Receptor Agonist Endomorphin 2 in Rat Brain Membranes

1998 ◽  
Vol 250 (3) ◽  
pp. 720-725 ◽  
Author(s):  
Mariana Spetea ◽  
Krisztina Monory ◽  
Csaba Tömböly ◽  
Géza Tóth ◽  
Eleni Tzavara ◽  
...  
Keyword(s):  
Rat Brain ◽  
Opioid Receptor ◽  
Receptor Agonist ◽  
The Novel ◽  
Brain Membranes ◽  
Opioid Receptor Agonist ◽  
Rat Brain Membranes ◽  
Μ Opioid Receptor

scholarly journals The novel μ-opioid receptor agonist PZM21 depresses respiration and induces tolerance to antinociception

2018 ◽  
Vol 175 (13) ◽  
pp. 2653-2661 ◽  
Author(s):  
Rob Hill ◽  
Alex Disney ◽  
Alex Conibear ◽  
Katy Sutcliffe ◽  
William Dewey ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonist ◽  
The Novel ◽  
Opioid Receptor Agonist ◽  
Μ Opioid Receptor

Opioids modulate N-methyl-D-aspartic acid (NMDA)-evoked responses of trigeminothalamic neurons

1996 ◽  
Vol 76 (3) ◽  
pp. 2093-2096 ◽  
Author(s):  
X. M. Wang ◽  
S. S. Mokha
Keyword(s):  
Nmda Receptor ◽  
Dorsal Horn ◽  
Aspartic Acid ◽  
Opioid Receptor ◽  
Receptor Agonist ◽  
Receptor Activation ◽  
Evoked Responses ◽  
Nociceptive Neurons ◽  
Nociceptive Transmission ◽  
Opioid Receptor Agonist

1. The present study investigated opioid-mediated modulation of N-methyl-D-aspartic acid (NMDA)-evoked responses of trigeminothalamic neurons in the superficial and deeper dorsal horn of the medulla (trigeminal nucleus caudalis) in rats anesthetized with urethane. 2. Microiontophoretic application of NMDA activated 18/19 trigeminothalamic neurons. Administration of [D-Ala2, N-Me-Phe4,Gly5-ol]-Enkephalin, a selective mu-opioid receptor agonist, reduced the NMDA-evoked responses in 77% of trigeminothalamic neurons. [D-Pen2,5]-Enkephalin, a selective delta-opioid receptor agonist, produced inhibition of NMDA-evoked responses in 36% of neurons. 3. We suggest that 1) NMDA-receptor activation excites trigeminothalamic nociceptive neurons and may, therefore, mediate nociceptive transmission in the medullary dorsal horn; and 2) the predominantly inhibitory modulation of NMDA-receptor-mediated responses of nociceptive trigeminothalamic neurons by activation of mu- and delta-opioid receptors may provide a neural mechanism for the antinociceptive actions of opioids.

scholarly journals Analgesic effects of a novel pH-dependent μ-opioid receptor agonist in models of neuropathic and abdominal pain

Pain ◽  
2018 ◽  
Vol 159 (11) ◽  
pp. 2277-2284 ◽  
Author(s):  
Antonio Rodriguez-Gaztelumendi ◽  
Viola Spahn ◽  
Dominika Labuz ◽  
Halina Machelska ◽  
Christoph Stein
Keyword(s):  
Abdominal Pain ◽  
Opioid Receptor ◽  
Receptor Agonist ◽  
Analgesic Effects ◽  
Opioid Receptor Agonist ◽  
Μ Opioid Receptor ◽  
Ph Dependent
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